Polyhydroxyethylaspartamide-based micelles for ocular drug delivery
Abstract
In this paper three copolymers of polyhydroxyethylaspartamide (PHEA), bearing in the side chains polyethylene glycol (PEG) and/or hexadecylamine (C(16)) (PHEA-PEG, PHEA-PEG-C(16) and PHEA-C(16) respectively) have been studied as potential colloidal drug carriers for ocular drug delivery. The physical characterization of all three PHEA derivatives, using the Langmuir trough (LT) and micellar affinity capillary electrophoresis (MACE) techniques allowed to assume that whereas alone PHEA backbone is an inert polymer with respect to the interactions with lipid membranes and drug complexation, when PHEA chains are grafted with long alkyl chains like C(16) or in combination C(16) chains and hydrophilic chains like PEG, copolymers with lipid membrane interaction ability and drug complexation capability are obtained. In vitro permeability studies performed on primary cultured rabbit conjunctival and corneal epithelia cells, using PHEA-C(16) and PHEA-PEG-C(16) as micelle carriers for netilmicin sulphate, dexamethasone alcohol and dexamethasone phosphate, demonstrated that in all cases drug loaded PHEA-C(16) and PHEA-PEG-C(16) micelles provide a drug permeation across ocular epithelia greater than simple drug solutions or suspensions. In particular PHEA-PEG-C(16) acts as the best permeability enhancer in our experimental model. In vivo bioavailability studies conducted with PHEA-PEG-C(16) micelles loaded with dexamethasone alcohol, confirmed that this system also provides a drug bioavailability greater in comparison with that obtained with water suspension of the same drug after ocular administration to rabbits.
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Metipranolol-loaded F127 micelle exhibited similar AUC to that of commercially available eye drops.
“In contrast, metipranolol-loaded F127 micelle exhibited similar AUC to that of commercially available eye drops.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [31]
In a recent study, chitosan/F127 micelles were fabricated for metipranolol at higher chitosan concentrations (0.3-0.8 %), and chitosan could enhance the metipranolol loading along with raised micelle zeta potential.
“In a recent study, chitosan/F127 micelles were fabricated for metipranolol at higher chitosan concentrations (0.3–0.8 %). At these concentrations, chitosan could enhance the metipranolol loading along with raised micelle zeta potential [31].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [31]
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“These results suggest that nanomicelles enhance the penetration of drug molecules through conjunctival epithelial cells to deep ocular tissue [31].”
- Authors
- Civiale, C., Licciardi, M., Cavallaro, G., Giammona, G., & Mazzone, M. G.
- Affiliations
- University of Palermo (IT)
- Corresponding author
- Giammona, G.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2009-08
- Volume
- 378
- Issue
- 1-2
- Pages
- 177-186
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2009209548
- Cited by
- 120
- References
- 29
- Citations by year
- 2026: 2 · 2025: 4 · 2024: 6 · 2023: 9 · 2022: 11 · 2021: 8 · 2020: 7 · 2019: 9 · 2018: 6 · 2017: 9 · 2016: 9 · 2015: 8 · 2014: 7 · 2013: 6 · 2012: 13
- FWCI
- 4.06
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Nova Science Publishers (Nova Science Publishers, Inc.) (submittedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Chemistry › Organic Chemistry › Surfactants and Colloidal Systems
- Keywords
- ocular drug delivery, micelles, PEGylation, membrane lipid interactions, drug complexation, ocular permeability, conjunctival epithelium, corneal epithelium, penetration enhancers, dexamethasone, bioavailability, Langmuir trough
- MeSH terms
- Administration, Topical, Amines, Animals, Biological Availability, Colloids, Conjunctiva, Dexamethasone, Drug Carriers, Hydrocarbons, Male, Micelles, Netilmicin, Peptides, Permeability, Polyethylene Glycols, Polymers, Rabbits, Epithelium, Corneal
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